Abstract

Synthesis and Anticonvulsant Activity of Thiadiazoles Derivatives

Author(s): Shweta Verma* and Asif Ali

Background: The derivatives of Thiadiazoles coupled with various benzaldehyde were synthesized. The synthesized derivatives were evaluated for different physicochemical parameters along with Log P values using different software programs to discover its ability to cross the blood brain barrier. The pharmacological activities such as anticonvulsant activity was evaluated by using PTZ method.

Objective: The new Thiadiazole derivatives were synthesized and assessed for different properties to predict its CNS activity. Thiosemicarbazide was used as a starting material which undergoes cyclization and then bromination to form the intermediate (C). The amino group of intermediates was allowed to react with different benzaldehydes to form the final product (D1-D5). The derivatives were evaluated for the anticonvulsant activity by using PTZ method.

Method: The starting reagent undergoes cyclization to form the product (B) which further undergoes bromination to form the intermediate (C). The intermediate then undergoes final step to form the derivatives in which amino group of intermediates was allowed to react with different benzaldehydes. The reactions of all the synthesized compounds were checked by TLC; final derivatives were purified by recrystallization and characterized by different spectroscopic methods. The similarity calculation and various physicochemical parameters were evaluated by using different software’s and then the derivatives were evaluated for anticonvulsant activity.

Result: The number of derivatives of Thiadiazole was synthesized and various physicochemical parameters were optimized which reveal that the compound containing methoxy group such as C2 and C5 exhibited significant potential when compared with the standard drug Sodium Valproate.

Conclusion: In conclusion, we have synthesized, evaluated various physicochemical parameters and anticonvulsant activity of new thiadiazole derivatives. The various derivatives were successfully synthesized and characterized by spectroscopic methods. It was identified that some derivatives have mild to moderate anticonvulsant activity. Nevertheless, the synthesis of these agents might be valuable in the future research and development for the development of the CNS active agents..

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